| Hazard Information | Back Directory | [Uses]
Akt3 degrader 1 (compound 12l) is a selective Akt3 degrader that overcomes Osimertinib.html" class="link-product" target="_blank">Osimertinib (HY-15772)-induced resistance in H1975OR NSCLC cells. Akt3 degrader 1 also has anti-proliferative activity and significantly inhibits tumour growth in mice. Akt3 degrader 1 can be used in the study of drug-resistant non-small cell lung cancer[1]. | [in vivo]
Akt3 degrader 1 (10, 20 mg/kg; i.p.; every 3 days for 5 weeks) induces significant tumor growth inhibition (TGI) with an approximately TGI value of 75% in mice[1]. | Animal Model: | NOD-SCID-IL2Rg-/-(NSI) mice (H1975OR xenograft model)[1]. | | Dosage: | 10, 20 mg/kg | | Administration: | Intraperitoneal administration; every 3 days for 5 weeks | | Result: | Inhibited tumor growth without causing obvious body weight loss or other signs of toxicity. |
| [References]
[1] Xu F, et al. Discovery of Isoform-Selective Akt3 Degraders Overcoming Osimertinib-Induced Resistance in Non-Small Cell Lung Cancer Cells. J Med Chem. 2022 Oct 27;65(20):14032-14048. DOI:10.1021/acs.jmedchem.2c01246 |
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